Synthesis of platinum(II) and palladium(II) complexes with 9,9-dihexyl-4,5-diazafluorene and their in vivo antitumour activity against Hep3B xenografted mice

Q.-W. Wang, P.-L. Lam*, R. S.-M. Wong, G. Y.-M. Cheng, K.-H. Lam, Z.-X. Bian*, C.-L. Ho*, Y.-H. Feng, R. Gambari, Y.-H. Lo*, W.-Y. Wong*, C.-H. Chui*

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

8 Citations (Scopus)
25 Downloads (Pure)

Abstract

Two complexes dichloro(9,9-dihexyl-4,5-diazafluorene)platinum(II) (Pt-DHF) and dichloro(9,9-dihexyl-4,5-diazafluorene)palladium(II) (Pd-DHF) were synthesized and their in vivo antitumour activity was investigated using an athymic nude mice model xenografted with human Hep3B carcinoma cells. Pt-DHF- and Pd-DHF-treated groups showed significant tumour growth inhibition (with about 9-fold and 3-fold tumour growth retardation) when compared with the vehicle control group. The liver toxicology effects on the animals of the two compounds were investigated. Pt-DHF and Pd-DHF-treated groups had a lower alanine transaminase and aspartate transaminase values than those of the vehicle treated group as the animals from the vehicle control group had very heavy hepatoma burden. We assume that both complexes could be further investigated as effective antitumour agents and it is worthwhile to study their underlying working mechanism.

Original languageEnglish
Pages (from-to)537-543
Number of pages7
JournalEuropean Journal of Medicinal Chemistry
Volume124
Early online date18 Aug 2016
DOIs
Publication statusPublished - Nov 2016

Scopus Subject Areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

User-Defined Keywords

  • Platinum-diazafluorene complex
  • Palladium-diazafluorene complex
  • Antitumour
  • In vivo

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